• 제목/요약/키워드: ${\beta}_2$-adrenergic Receptor

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돼지 분만 시기의 조절에 관하여;IV. 자궁 평활근의 운동성에 대한 APT의 영향 (Control of Parturition Time on Pig;IV. Effect of ATP on Uterine Smooth Muscle Motility)

  • 박상은;황보원;변유성;조광제
    • 한국동물위생학회지
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    • 제19권2호
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    • pp.154-162
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    • 1996
  • The effcets of adenosine 5'-triphosphate(ATP) were investigated on the uterine smooth muscle motility in the pig. The results were summarized as follows: 1. The effects of the porcine uterine smooth muscle and the contractile responses increased between the concentration of ATP $10^{-5}$ and $10^{-3}$ M with a dose-dependent manner. 2. The contractile response induced by ATP($10^{-4}$ M) was not blocked by pretreatment with cholinergic receptor blocker, atropine ($10^{-6}$ M) 3. The contractile response induced by ATP ($10^{-4}$ M) was not blocked by pretreatment with $\alpha$ -adrenergic receptor blocker, phentolamine(10$^{-6}$ M) and ${\beta}$-adrenergic blocker, propranolol ($10^{-6}$ M). 4. The contractile response induced by ATP($10^{-4}$ M) was not appeared in 4Ca^{++}$ -free medium. As the concentration of $Ca^{++}$ in $Ca^{++}$ -free medium was increased, the contractile response induced by ATP ($10^{-4}$ M) was enhenced but was completely inhibited by pretreatment with $Ca^{++}$ -channel blocker, papaverine($10^{-6}$ M) or verapamil($10^{-6}$ M). From these results, it was conclued that the effects of ATP were the contraction mediated by purinergic receptor in uterine smooth muscle of pig.

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베타 2-아드레날린 수용체의 유전자 변이형이 비만도에 미치는 영향 (Effects of ${\beta}2-Adrenergic$ Receptor Polymorphism on Obesity)

  • 김길수;오현희;최선미;양현성;배정환;윤유식
    • 한방비만학회지
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    • 제3권1호
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    • pp.7-16
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    • 2003
  • Objectives : The lipolytic effects of catecholamines in adipose tissue are mediated by members of adrenergic receptors. This study was conducted to examine the effects of ${\beta}2-AR$ Gln27Glu (Q27E) polymorphism on obesity indices and risk among obesity clinic patients. Methods : 532 subjects, 38 men and 494 women, who attended a weight loss program in a local obesity clinic were analyzed. Height, weight, BMI, WHR and obesity index were measured or calculated. Body composition was measured by bio-impedance analysis. Genotype of ${\beta}2-AR$ polymorphism in codon 27 was analyzed by PCR-RFLP method. Serum concentrations of fasting glucose, total and HDL cholesterol, and triglyceride were determined by autobiochemical analyzer. Results: The Genotype distributions of ${\beta}2-AR$ gene were QQ type 81.3%, QE type 17.9% and EE type 8%. Therefore, the frequency of E allele of ${\beta}2-AR$ gene was 0.170 in the total subjects. The frequency of the ${\beta}2-AR$ variant genotype(QE+EE) was significantly higher in obese group($BMI{\geqq}25$) compared with non-obese group(p=0.027). Weight was significantly higher in variant(QE+EE) type compared with normal(QQ) type in total subjects(p=0.001), male(p=0.022) and female(p=0.013). BMI, obesity index and WHR were also significantly higher in QE+EE type. Body fat man was significantly higher in QE+EE type in total subjects(p=0.005) and female(p=0.027). When forward stepwise regression analysis was used to create a model of risk predictors of obesity($BMI{\geqq}25$), QE+EE type of ${\beta}2-AR$ gene was found to be a significant risk factor for obesity (p=0.042, ORs 1.597). Conclusions: QE+EE genotype of ${\beta}2-AR$ was associated with increased obesity indices and might be a significant risk factor for obesity.

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Adrenergic receptor β2 activation by stress promotes breast cancer progression through macrophages M2 polarization in tumor microenvironment

  • Qin, Jun-fang;Jin, Feng-jiao;Li, Ning;Guan, Hai-tao;Lan, Lan;Ni, Hong;Wang, Yue
    • BMB Reports
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    • 제48권5호
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    • pp.295-300
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    • 2015
  • Stress and its related hormones epinephrine (E) and norepinephrine (NE) play a crucial role in tumor progression. Macrophages in the tumor microenvironment (TME) polarized to M2 is also a vital pathway for tumor deterioration. Here, we explore the underlying role of macrophages in the effect of stress and E promoting breast cancer growth. It was found that the weight and volume of tumor in tumor bearing mice were increased, and dramatically accompanied with the rising E level after chronic stress using social isolation. What is most noteworthy, the number of M2 macrophages inside tumor was up-regulated with it. The effects of E treatment appear to be directly related to the change of M2 phenotype is reproduced in vitro. Moreover, E receptor $ADR{\beta}2$ involved in E promoting M2 polarization was comprehended simultaneously. Our results imply psychological stress is influential on specific immune system, more essential for the comprehensive treatment against tumors. [BMB Reports 2015; 48(5): 295-300]

Higenamine의 합성 및 가토의 심혈관계에 미치는 영향 : 베타-아드레날린성 효능 약물 (Synthesis of Higenamine and its Cardiovascular Effects in Rabbit: Evidence for ${\beta}-Adrenoceptor$ agonist)

  • 장기철;임정규;박찬웅
    • 대한약리학회지
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    • 제22권2호
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    • pp.96-104
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    • 1986
  • 최근에 미나라아제비과 (Ranunculaceae)에 속하는 부자(Aconiti tuber)로부터 강심작용을 나타내는 성분을 분리하여 Higenamine이라 명명하였고 그 작용기전을 밝히려는 시도가 활발히 진행되고 있다. 그러나 생약제로 부터 얻을 수 있는 Higenamine은 극히 미량이고 그 과정 또한 복잡하다. 따라서 본 연구에서는 유효성분을 대량 얻기 위한 방법으로서 전합성(total Synthesis)을 시도하였으며 IR, UV, NMR 및 elemental 분석등을 통하여 합성된 물질을 확인하였으며 가토에 대하여 in vivo에서 혈압, 심박동수, 호흡 및 말초저항에 미치는 영향과 아울러 in vitro에서 심근수축 증강작용(positive inotropic action) 및 심박속도 증강작용(positivechronotropic action)을 관찰 분석하여 다음과 같은 결론을 얻었다. 1) Higenamine은 $1-10\;{\mu}g/kg/min$ 정맥주사시 수축기 및 이완기혈압 모두를 용량 의존적으로 하강시켰고 후자가 전자보다 더욱 현저하였으며 호흡은 촉진되었고 말초 혈류량은 증가되었으나 심박동수는 영향이 없었다. 2) 혈압에 대한 Higenamine의 작용은 propranolol 전처치에 의하여 억제되었다. 3) Higenamine의 catechol핵과 커다란 아미노기는 베타 수용체기 대하여 전자는 활성을 후자는 친화력과 관계있을 것으로 추정하였다. 이상의 결과 Higenamine은 adrenergic ${\beta}$-수용체에 작용하여 그 작용을 발휘하는 것으로 사료 되었다.

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해명 회장 운동에 대한 아드레나린성 ${\alpha}$-수용체에 관한 연구 (Studies on the Adrenergic Alpha-Receptor in the Guinea Pig Ileum)

  • 고창만
    • 대한약리학회지
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    • 제19권1호
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    • pp.85-92
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    • 1983
  • Intestine is innervated by an interconnected plexus of both sympathetic and parasympathetic nerve fibers. Sympathetic influence causes inhibition of intestinal motility mediated by both ${\alpha}-\;and\;{\beta}-adrenergic$ receptors. The mechanism of intestinal relaxation by ${\beta}-receptors$ has been extensively studied, but the function of ${\alpha}-receptors$ in intestinal motility is still unclear. Although it is suggested that catecholamine reduces acetylcholine release and this may play an important role in ${\alpha}-receptor$ mediated intestinal relaxation, there is no definite evidences about the mechanism and site of action of ${\alpha}-receptor$ mediated relaxation. In this experiment, therefore, the effect and site of action of ${\alpha}-receptor$ agonists were investigated in the guinea pig ileum using electrical field stimulation. The results are summarized as follows : 1) Electrical field stimulation elicited tonic contraction in isolated guinea pig ileum ana this contraction was completely inhibited by the pretreatment of tetrodotoxin or atropine. 2) Norepinephrine, epinephrine and dopamine inhibited the contraction induced by electrical field stimulation but methoxamine and phenylephrine had little effects. 3) Inhibitory effects of norepinephrine and dopamine was partially blocked by yohimbine and phentolamine pretreatment. But haloperidol and propranolol pretreatment cause no effects on the electrical field stimulation induced contraction. Inhibitory effect of dopamine was completely blocked by both haloperidol and yohimbine pretreatment. 4) Inhibitory effects of norepinephrine and dopamine were little affected by the pretreatment with hexamethonium. It is suggested that electrical field stimulation causes tonic contraction of guinea pig ileum by releasing acetylcholine from postganglionic fiber, and this release is blocked by presynaptic ${\alpha}-receptor$ activation.

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Higenamine의 Guinea pig 기관 평활근 이완작용 (Bronchodilator Effect of Higenamine in Isolated Guinea-pig Tracheal Smooth Muscle)

  • 윤효인;장기철;홍성근;이창업
    • 대한수의학회지
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    • 제27권1호
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    • pp.35-40
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    • 1987
  • Higenamine, a benzyltetrahydroisopuinoline analog isolated from aconite tuber, has potent isotropic action. Recent studies suggest it may have beta receptor agonistic property in that its inotropic action is blocked by propranolol in isolated rabbit heart. However, no study has been carried out on other organs than heart. Higenamine is expected to have pharmacological actions on smooth muscle on the ground that it has catecholamine moiety and tetrahydrosioquinoline nucleus in its chemical structure, both of which are well known to have smooth muscle relaxation effects. Therefore present study was aimed at determining whether higenamine has bronchodilating effect in isolated guinea pig trachea smooth muscle rich in adrenergic beta receptor and if any, it has agonistic effect on beta receptor. The results were summarized as follows : 1. Higenamine had remarkable bronchodilating effect in guinea pig tracheal smooth muscle in a dose-dependent manner. 2. Bronchodilator effect of higenamine in isolated guinea pig tracheal smooth muscle was blocked competitively by propranolol. The $pD_2$ value of higenamine in isolated guinea pig tracheal smooth muscle was 5.65 and the $pA_2$ value of propranolol against higenamine in the same preparation was 7.97.

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인체 정관의 약리학적 검색 -아드레날린성 및 콜린성 수용체의 공존과 Diazepam의 작용- (Pharmacological Studies on Human Vas Deferens -Coexistence of Adrenergic and Cholinergic Receptors, and Effect of Diazepam-)

  • 김원준;이광윤;하정희;박동춘
    • 대한약리학회지
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    • 제24권2호
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    • pp.189-195
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    • 1988
  • 인체 정관 평활근에서 각종 자율신경전달체 수용체의 유무를 조사하고 benzodiazepine계의 진정-항불안제인 diazepam이 평활근 운동성에 미치는 작용을 관찰하기 위하여, 32내지 45세의 건강한 지원자로부터 정관절편을 얻었다. 정관 절제술은 국소마취하에 시행되었고, 정관절편의 수축력 측정은 등장성장력측정기에 의하였다. 적출장기실험조 내에서 정관절편의 자율수축은 관찰되지 않았으나, norepinephrine에 대한 반응성은 $33^{\circ}C$에서 가장 예민하였던 바, 이 norepinephrine에 의한 농도의존적 수축력증가작용은 알파-아드레날린성 차단제인 phentolamine에 의해 억제되었다. 또 인체 정관절편은 본 실험의 조건하에서 isoproterenol 의하여 수축하였고, 이 수축작용은 베타-아드레날린성 차단제인 propranolol 의하여 완전히 제거되었다. 동시에 인체 정관절편은 acetylcholine에의해서도 비교적 강하게 수축하였고, 이 수축작용은 콜린성 무스카린성 차단제인 atropine에 의하여 완전히 억제되었다. Diazepam은 norepinephrine에 의한 수축을농도 의존적으로 억 제 하였다. 이상의 결과를 종합하면, 인체 정관 평활근은 체온보다 낮은 $33^{\circ}C$에서 그 활동성이 가장 강하고, 자율신경에 대하여서는 아드레날린성 및 콜린성 수용체가 공존하고 있으며, diazepam은 그 수축력을 약화시킨다고 사료된다.

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돼지 적출 신동맥에 대한 adenosine triphosphate의 영향과 Ca++의 동원 (Source of Ca++ and effect of adenosine triphosphate on the isolated renal artery of pig)

  • 남윤정;김주헌
    • 대한수의학회지
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    • 제31권3호
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    • pp.253-258
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    • 1991
  • The aims of this study were to investigate the effect of adenosine triphosphate (ATP), which has been known as the neurotransmitter of nonadrenergic, noncholinergic nerves, and the source of $Ca^{\sharp}$ in the effect of ATP on the isolated renal artery of pig. The results of this study were summarized as follows: 1. ATP caused the contraction and the contractile responses were increased in a dose-dependent manner between the concentration of ATP $2{\times}10^{-3}M$ and $10^{-2}M$ on the isolated renal artery of pig. 2. The contractile responses induced by ATP $(5{\times}10^{-3}M)$ were not blocked by pretreatment with cholinergic receptor blocker (atropine, $10^{-6}M$), $\alpha$-adrenergic recptor blocker(phentolamine, $10^{-6}M$) or $\beta$-adrenergic receptor blocker (propranolol, $10^{-6}M$), and $H_1$-receptor blocker (pyrilamine, $10^{-6}M$) or $H_2$-receptor blocker (cimetidine, $10^{-6}M$) on the isolated renal artery of pig. 3. The contractile responses induced by ATP $(5{\times}10^{-3}M)$ were not appeared in $Ca^{\sharp}$-free medium. As the concentration of $Ca^{\sharp}$ in $Ca^{\sharp}$-free medium was increased, the contractile responses induced by ATP $(5{\times}10^{-3}M)$ were enhanced but were completely inhibited by pretreatment with $Ca^{\sharp}$-channel blocker, papaverine $(5{\times}10^{-5}M)$ or verapamil $(5{\times}10^{-5}M)$ on the isolated renal artery of pig.

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한국인에서 ${\beta}_3AR$, UCP2 유전자의 다형성과 체질량지수의 관련성 (Association Analyses of ${\beta}_3AR$ Trp64Arg and UCP-2 -866G/A Polymorphisms with Body Mass Index in Korean)

  • 정홍수;이주현;사공준;배성욱;김정희;김재룡
    • Journal of Yeungnam Medical Science
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    • 제24권2호
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    • pp.252-261
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    • 2007
  • 비만은 서구와 우리나라에서 가장 흔한 영양 관련 질환이며, 유전적, 환경적, 생활습관인자들에 의해 초래된다. 이 연구에서는 성인750명을 대상으로 ${\beta}_3AR$ Trp64Arg, UCP2 -866G/A 유전자 다형성을 PCR-RFLP법으로 조사한 후, 체질량지수와 비교하여 어떤 유전자의 다형성이 비만과 관련 있는지 분석하였다. ${\beta}_3AR$의 Trp64Arg의 다형성 분포는 Arg64Arg의 경우 체질량지수 27이상인 비만인에서만 관찰되었지만, 전체적으로 비만인과 정상인에서 통계적으로 유의한 차이가 없었다. UCP2 -866G/A 다형성의 분포는 G/A의 경우 비만인 에서, A/A의 경우 정상인에서 더 통계적으로 유의하게 높았다(p<0.05). 이상의 결과로부터 ${\beta}_3AR$ Trp64Arg 다형성에 비해 UCP2 -866G/A 다형성이 한국인에서 비만과 비만관련 질병을 예측하는데 더 유용한 것으로 판단된다.

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Expression of neurotransmitter receptors in oral keratinocytes and their response to agonists

  • Choi, Eun Ji;Chang, Sung-Ho;Choi, Se-Young;Choi, Youngnim
    • International Journal of Oral Biology
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    • 제46권1호
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    • pp.39-44
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    • 2021
  • This study aimed to investigate whether neurotransmitter receptors in the nervous system were also expressed in oral keratinocytes. Expressions of various neurotransmitter receptor genes in immortalized mouse oral keratinocyte (IMOK) cells were examined by reverse transcriptase polymerase chain reaction. IMOK cells expressed calcitonin gene-related peptide (CGRP) receptor subunit genes Ramp1 and Ramp3 and glutamate receptor subunit genes Grina, Gria3, Grin1, Grin2a, and Grin2d. Moreover, IMOK cells expressed Adrb2 and Chrna5 that encode beta 2 adrenergic receptor and cholinergic receptor nicotinic alpha 5 for sympathetic and parasympathetic neurotransmitters, respectively. The expression of Bdkrb1 and Ptger4, which encode receptors for bradykinin and prostaglandin E2 involved in inflammatory responses, was also observed at low levels. Expressions of Ramp1 and Grina in the mouse gingival epithelium were also confirmed by immunohistochemistry. When the function of neurotransmitter receptors expressed on IMOK cells was tested by intracellular calcium response, CGRP, glutamate, and cholinergic receptors did not respond to their agonists, but the bradykinin receptor responded to bradykinin. Collectively, oral keratinocytes express several neurotransmitter receptors, suggesting the potential regulation of oral epithelial homeostasis by the nervous system.